1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Apoptosis
  2. HSP
    Apoptosis
  3. YUM70

YUM70 

Cat. No.: HY-138364
Handling Instructions

YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model.

For research use only. We do not sell to patients.

YUM70 Chemical Structure

YUM70 Chemical Structure

CAS No. : 423145-35-1

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5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
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25 mg USD 1100 In-stock
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50 mg USD 1700 In-stock
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100 mg USD 2500 In-stock
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Description

YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model[1].

IC50 & Target

IC50: 1.5 μM (glucose-regulated protein 78)[1]

In Vitro

YUM70 shows selective cytotoxicity for MIA PaCa-2, PANC-1, BxPC-3 cells (IC50=2.8, 4.5, and 9.6 μM, respectively) over normal pancreatic tissue-derived HPNE cells (IC50>30 μM)[1].
YUM70 (5 μM; 24 h) induces endoplasmic reticulum (ER) stress-mediated apoptosis of MIA PaCa-2cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2, PANC-1 cells
Concentration: 0.1, 1, 2.5, 5, 10 μM
Incubation Time: 2, 4, 8, 24, 48 hours
Result: Increased the protein levels of FAM129A, DDIT3, CHAC-1, DDIT4, UPP1, and GRP78 in a dose- and time-dependent manner.
In Vivo

YUM70 (30 mg/kg; i.p. 5 days a week for 7 weeks) inhibits tumor growth in a MIA PaCa-2 xenograft model[1].
YUM70 (15 mg/kg; i.v.) exhibits t1/2 (1.40 h), CL (724.04 mL/h/kg), and Vss (1162.73 mL/kg) in mice[1].
YUM70 (30 mg/kg; p.o.) exhibits bioavailability (6.71%), t1/2 (2.74 h), and CL (9230.15 mL/h/kg) in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-week old female NCr nude mice were injected with MIA PaCa-2 cells[1]
Dosage: 30 mg/kg
Administration: I.p. 5 days a week for 7 weeks
Result: Observed a significant tumor growth delay with no significant change in body weight during the course of treatment.
Molecular Weight

398.84

Formula

C₂₁H₁₉ClN₂O₄

CAS No.

423145-35-1

SMILES

CCCC(NC(C1=CC=C(OCO2)C2=C1)C3=CC(Cl)=C4C=CC=NC4=C3O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (250.73 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5073 mL 12.5364 mL 25.0727 mL
5 mM 0.5015 mL 2.5073 mL 5.0145 mL
10 mM 0.2507 mL 1.2536 mL 2.5073 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.27 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

YUM70YUM 70YUM-70HSPApoptosisHeat shock proteinsglucose-regulatedprotein78GRP78endoplasmicreticulumERstress-mediatedapoptosispancreaticcancerInhibitorinhibitorinhibit

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YUM70
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